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Results for "

negative+allosteric+modulator

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (1) Adrenergic Receptor (1) Amino Acid Derivatives (1) Apoptosis (2) Bacterial (1) Calcium Channel (1) Cannabinoid Receptor (1) CaSR (3) CCR (1) Dopamine Receptor (1) Drug Derivative (1) Drug Intermediate (1) Drug Isomer (1) Endogenous Metabolite (1) ERK (3) Estrogen Receptor/ERR (2) GABA Receptor (7) GCGR (2) Histone Methyltransferase (2) HSV (1) iGluR (12) Interleukin Related (1) LPL Receptor (1) mAChR (5) mGluR (50) Molecular Glues (1) P2X Receptor (3) PERK (1) Phosphodiesterase (PDE) (1) Potassium Channel (3) Proteasome (1) Reference Standards (9) Src (1) TRP Channel (1) Urotensin Receptor (1) Wnt (1) β-catenin (1)
By Research Areas:	Cancer (9) Cardiovascular Disease (3) Endocrinology (1) Infection (1) Inflammation/Immunology (7) Metabolic Disease (9) Neurological Disease (78)

By Targets:

5-HT Receptor (1)

Adrenergic Receptor (1)

Amino Acid Derivatives (1)

Apoptosis (2)

Bacterial (1)

Calcium Channel (1)

Cannabinoid Receptor (1)

CaSR (3)

CCR (1)

Dopamine Receptor (1)

Drug Derivative (1)

Drug Intermediate (1)

Drug Isomer (1)

Endogenous Metabolite (1)

ERK (3)

Estrogen Receptor/ERR (2)

GABA Receptor (7)

GCGR (2)

Histone Methyltransferase (2)

HSV (1)

iGluR (12)

Interleukin Related (1)

LPL Receptor (1)

mAChR (5)

mGluR (50)

Molecular Glues (1)

P2X Receptor (3)

PERK (1)

Phosphodiesterase (PDE) (1)

Potassium Channel (3)

Proteasome (1)

Reference Standards (9)

Src (1)

TRP Channel (1)

Urotensin Receptor (1)

Wnt (1)

β-catenin (1)

By Research Areas:

Cancer (9)

Cardiovascular Disease (3)

Endocrinology (1)

Infection (1)

Inflammation/Immunology (7)

Metabolic Disease (9)

Neurological Disease (78)

103

Inhibitors & Agonists

Peptides

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-16716

Basmisanil 1 Publications Verification RG1662; RO5186582	GABA Receptor	Neurological Disease
Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a K_i value of 5 nM and IC₅₀ value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .

HY-173156

UNC10013	Histone Methyltransferase	Cancer
UNC10013 is an inhibitor targeting the triple Tudor domain (3TD) of SETDB1. UNC10013 covalently binds to Cys385 of SETDB1 3TD, acts as a negative allosteric modulator of the methyltransferase domain of SETDB1, reduces the level of Akt methylation mediated by SETDB1, and blocks Tyr308 phosphorylation of Akt. UNC10013 is applicable to cancer-related research .

HY-122138

VU6010572 1 Publications Verification	mGluR	Neurological Disease
VU6010572 is a potent, selective and brain-penetrant mGlu3 negative allosteric modulator with IC₅₀ of 245 nM. VU6010572 is highly CNS penetrant .

HY-124622

NNC-0640	GCGR	Metabolic Disease
NNC-0640 is an effective negative allosteric modulator (NAM) of the human glucagon receptor (GCGR), with an IC₅₀ value of 69.2 nM. NNC-0640 holds potential for research in the field of diabetes .

HY-15446

Basimglurant 1 Publications Verification RG7090; RO4917523	mGluR	Neurological Disease
Basimglurant (RG7090; RO4917523) is a selective, orally active, blood-brain barrier permeable negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5), with a K_i of 1.4 nM (against [ ³H]-ABP688 (HY-110141)) and 35.6 nM (against [ ³H]-MPEP (HY-14609A)). Basimglurant inhibits mGlu5-mediated signaling pathways and receptor constitutive activity, regulates dopamine levels in the nucleus accumbens, exerts anxiolytic, antidepressant-like, analgesic and arousal-promoting effects, and alters δ-wave power during non-rapid eye movement sleep. Basimglurant can be used in research on depression, fragile X syndrome, anxiety disorders, etc .

HY-108710

VU0650786 2 Publications Verification	mGluR	Neurological Disease
VU0650786 is a potent and selective CNS penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM), with an IC₅₀ of 392 nM. VU0650786 has antidepressant and anxiolytic activity in rodents .

HY-14859

Dipraglurant ADX48621	mGluR	Neurological Disease
Dipraglurant (ADX48621) is a potent, selective, orally active and brain penetrant mGluR5 negative allosteric modulator (NAM), with an IC₅₀ of 21 nM. Dipraglurant can reduce Levodopa-induced dyskinesia (LID) in vivo . Dipraglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-101845

FITM 1 Publications Verification	mGluR	Cancer
FITM is a negative allosteric modulator of mGlu1 receptor with a K_i of 2.5 nM.

HY-124803

*GPCR modulator-1*	GCGR	Metabolic Disease
GPCR modulator-1 is a negative allosteric modulator of the GLP-1 receptor (GLP-1R). GPCR modulator-1 can be used for the study of type 2 diabetes .

HY-135891

AZD2423	CCR	Neurological Disease
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC₅₀ of 1.2 nM for CCR2 Ca ²⁺ flux .

HY-103320A

Calhex 231 hydrochloride Maximum Cited Publications 6 Publications Verification	CaSR	Metabolic Disease
Calhex 231 hydrochloride is a potent negative allosteric modulator that blocks (IC₅₀ = 0.39 μM) increases in [ ³H]inositol phosphates elicited by activating the human wild-type CaSR transiently Ca ²⁺-sensing receptor. Calhex 231 hydrochloride can be used in the study of traumatic hemorrhagic shock (THS) and diabetic cardiomyopathy (DCM) .

HY-116553

FzM1	Wnt β-catenin	Cancer
FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC_50inh=?6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade .

HY-16766

Decoglurant RO4995819	mGluR	Neurological Disease
Decoglurant (RO4995819) is a negative allosteric modulator of mGluR2 and mGluR3. Decoglurant is developed as an antidepressant .

HY-129946

Dopamine D2 receptor antagonist-1	Dopamine Receptor	Neurological Disease
Dopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity .

HY-110278

ADX71743	mGluR	Neurological Disease
ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 can cross the blood-brain barrier (BBB) and possesses anxiolytic activity. .

HY-117959

TAK-615	LPL Receptor	Inflammation/Immunology
TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (K_d high affinity of 1.7 nM and K_d low affinity of 14.5 nM) .

HY-12567

ML375 VU0483253	mAChR	Neurological Disease
ML375 (VU0483253) is a potent, highly selective, brain-penetrant and orally active M5 mAChR negative allosteric modulator (NAM) with IC₅₀s of 300 nM and 790 nM for human and rat M5, respectively. ML375 is inactive at human and rat M1-M4 .

HY-145585

Onfasprodil MIJ-821	iGluR	Neurological Disease
Onfasprodil (MIJ-821) is a selective intravenous NMDA receptor NR2B subunit negative allosteric modulator (NAM). Onfasprodil inhibits the activity of NR2B-NMDA receptors. Onfasprodil has a rapid antidepressant effect. Onfasprodil can be used for the research of treatment-resistant depression (TRD) .

HY-19630

ML289 VU0463597	mGluR	Neurological Disease
ML289 (VU0463597) is a potent, selective, and CNS-penetrant mGlu3 (IC₅₀=0.66 μM) negative allosteric modulator. ML289 displays >15-fold selectivity over mGlu2 and is inactive against mGlu5 . ML289 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-178121

JNJ-78911118	iGluR	Neurological Disease Inflammation/Immunology
JNJ-78911118 is a potent, brain-penetrant, selective GluN2A antagonist (IC₅₀ = 44 nM). JNJ-78911118 shows >200-fold selectivity against GluN1/2B, 2C and 2D receptors. JNJ-78911118 functions as a negative allosteric modulator (NAM) by insurmountably suppressing glutamate efficacy and reducing glycine potency at GluN1/2A receptors. JNJ-78911118 produces profound pharmacodynamic effects in vivo. JNJ-78911118 can be used for depression research .

HY-168992

UNC6535	Histone Methyltransferase	Neurological Disease Cancer
UNC6535 is a covalent ligand targeting the SETDB1 triple Tudor domain (3TD) with negative allosteric modulator properties, with an IC₅₀ of 3.4 μM and a K_d of 4.2 μM. UNC6535 inhibits the methyltransferase activity of recombinant SETDB1 protein lacking the 3TD domain. UNC6535 reversibly binds to the aromatic cages of both TD2 and TD3 subdomains of SETDB1 3TD simultaneously, displacing the endogenous H3K9Me2K14Ac histone tail ligand. UNC6535 can be used in research on cancer and neurodegenerative diseases .

HY-114403

VU6012962	mGluR	Neurological Disease
VU6012962 is an orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu₇ NAM) with an IC₅₀ of 347 nM .

HY-101281

VU 6008667	mAChR	Neurological Disease
VU 6008667 is a selective negative allosteric modulator of M5 NAM with IC₅₀s of 1.2 μM and 1.6 μM for human M5 and rat M5, respectively. High CNS penetration .

HY-164764

ADX61623	Estrogen Receptor/ERR	Endocrinology
ADX61623 is a potent follicle stimulating hormone (FSH) receptor (FSHR) negative allosteric modulator (NAM). ADX61623 shows luteinizing hormone receptor (LH-R) activity and is not active on thyroid-stimulating hormone (TSH) receptors. ADX61623 can be used for the study of estrogen dependent disease .

HY-W101299

*N-Acetyl-D-allo-isoleucine*	Amino Acid Derivatives	Metabolic Disease
N-Acetyl-D-allo-isoleucine is an amino acid derivative. N-Acetyl-D-allo-isoleucine is promising for research of amino acid metabolism, such as abnormal isoleucine metabolism .

HY-155811

DQP-997-74	iGluR	Neurological Disease
DQP-997-74 (compound 2i) is a selective negative allosteric modulator of N-methyl-d-aspartate receptor (NMDAR), specifically targeting GluN2C/D (IC₅₀: 0.069 μM and 0.035 μM), with blood-brain barrier penetrability. Where DQP refers to dihydroquinoline-pyrazoline. DQP-997-74 acts synergistically with the agonist glutamate to exhibit time-dependent enhanced potency in inhibiting hypersynchronous activity driven by high-frequency excitatory synaptic transmission. DQP-997-74 reduces the number of epileptogenesis in a murine model of tuberous sclerosis complex (TSC)-induced epilepsy. DQP-997-74 can be used for research on NMDAR-related neurological diseases .

HY-155088

MK-8768	mGluR	Metabolic Disease
MK-8768 is a highly potent, orally bioavailable and selective class of mGluR2 *negative allosteric* modulator (IC₅₀ of 9 .6nM) with excellent brain permeability.

HY-129636

CLH304a (E)-GABAB receptor antagonist 1	GABA Receptor ERK	Neurological Disease
CLH304a (compound 14) is a specific and noncompetitive GABA_B receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC₅₀ of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABA_B receptor .

HY-19888

GSK-1482160	P2X Receptor Interleukin Related	Neurological Disease Inflammation/Immunology
GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC₅₀s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI) .

HY-168758

Delta3,5-cholestadien-7-one	GABA Receptor	Neurological Disease
Delta3,5-cholestadien-7-one is an oxysterol and a negative allosteric modulator of GABAA receptors. Delta3,5-cholestadien-7-one reduces GABA-induced currents in HEK cells expressing α1β1γ2 or α4β3γ2 subunit-containing GABAA receptors with IC₅₀ values of 1.5 and 1 µM, respectively. Delta3,5-cholestadien-7-one reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons .

HY-103574

Raseglurant hydrochloride ADX-10059 hydrochloride	mGluR	Neurological Disease
Raseglurant hydrochloride is a negative allosteric modulator of mGluR5. Raseglurant hydrochloride can be used in study migraine .

HY-120375

LUF7346	Potassium Channel	Cardiovascular Disease
LUF7346 is a potent Kv11.1 (hERG) channel negative allosteric modulator, with an IC₅₀ of 35.6 ± 3.2 nM .

HY-133555

mGluR2 antagonist 1	mGluR	Neurological Disease
mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC₅₀ of 9 nM) with excellent brain permeability .

HY-177127

Satoprodil	iGluR	Neurological Disease
Satoprodil (example 2) is a potent N-methyl-D-aspartate (NMDA) receptor negative allosteric modulator with an IC₅₀ value of 123 nM for NR2B .

HY-14866

Raseglurant ADX-10059	mGluR	Neurological Disease
Raseglurant (ADX-10059) is a mGlu5 receptor negative allosteric modulator. Raseglurant is effective against migraine. Raseglurant reduces the Haloperidol (HY-14538)-induced catalepsy in mice .

HY-101281A

(Rac)-VU 6008667	mAChR	Neurological Disease
(Rac)-VU 6008667 is a selective negative allosteric modulator of muscarinic acetylcholine receptor subtype 5 (M5 NAM) (IC₅₀=1.8 μM, pIC₅₀= 5.75), has high CNS penetration .

HY-103572

MNI137	mGluR	Neurological Disease
MNI137 is a potent and selective negative allosteric modulator for group II mGluRs. MNI137 has IC₅₀s values of 8.3 and 12.6 nM for human and rat mGlu2 inhibition of glutamate-induced calcium mobilization .

HY-107509

LY2389575 hydrochloride	mGluR	Neurological Disease
LY2389575 hydrochloride is a selective and noncompetitive mGlu3 negative allosteric modulator (NAM), with an IC₅₀ value of 190 nM. LY2389575 hydrochloride induces an increase in Mrc1 levels. LY2389575 hydrochloride also independently amplifies Amyloid beta (Aβ) toxicity and can be used in study of Alzheimer's disease .

HY-124985

VU6010608	mGluR	Neurological Disease
VU6010608 is a blood-brain barrier-crossing mGlu7 negative allosteric modulator (IC₅₀ = 0.76 μM). VU6010608 can block long-term enhancement (LTP) of SC-CA1 synapses in mouse brain slices induced by high-frequency stimulation. VU6010608 can be used for research on neurological diseases .

HY-15469

GW791343 dihydrochloride 1 Publications Verification	P2X Receptor	Neurological Disease
GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC₅₀ of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease .

HY-103118

PU02	5-HT Receptor Apoptosis	Neurological Disease Cancer
PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT₃ receptor, with IC₅₀ values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT₃A and 5-HT₃AB receptors respectively .

HY-119282

AZD6538	mGluR	Neurological Disease
AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG (HY-12598A)-stimulated intracellular Ca2+ release in HEK cells expressing rat or human mGluR5, with IC₅₀ values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain .

HY-179226

AP-7-168	Molecular Glues Adrenergic Receptor	Inflammation/Immunology
AP-7-168, molecular glues, is a β-arrestin-biased negative allosteric modulator of the β2-adrenergic receptor (β2AR). AP-7-168 can promote β2AR homodimerization and inhibit GRK5-mediated β2AR phosphorylation. AP-7-168 can sustain bronchorelaxation in cell and tissue. AP-7-168 can be used for the researches of inflammation and immunology, such as asthma .

HY-112788

ONO-8590580	GABA Receptor	Neurological Disease
ONO-8590580 is a GABA_A α5 negative allosteric modulator.

HY-110191

VU0469650	mGluR	Neurological Disease Cancer
VU0469650 is a potent, selective and brain-penetrant negative allosteric modulator of mGlu₁ receptor, with an IC₅₀ of 99 nM .

HY-100667

UBP608 1 Publications Verification	iGluR	Neurological Disease
UBP608 is a potent N-Methyl-D-aspartate receptors (NMDARs) negative allosteric modulator. UBP608 has the potential for the research of neurological disorders .

HY-124393

GRN-529	mGluR	Neurological Disease
GRN-529 is a negative allosteric modulator (NAM) for mGluR5. GRN-259 modulates sleep-wake activity, and exhibits anxiolytic efficacy in rats .

HY-114863

PHCCC(4Me) THCCC	mGluR	Neurological Disease
PHCCC(4Me) (THCCC), a PHCCC analog, is a dual mGluR2 (IC₅₀ of 1.5 μM) negative allosteric modulator and mGluR3 (EC₅₀ of 8.9 μM) positive allosteric modulator .

HY-107774

BMS-986163	iGluR	Neurological Disease
BMS-986163 is a negative allosteric modulator of GluN2B. The proagent BMS-986163 rapidly converts to its active parent molecule BMS-986169 (K_i=4 nM, IC₅₀=24 nM).

HY-115483

VU0477573	mGluR	Neurological Disease
VU0477573 is a brain-penetrant partial negative allosteric modulator of metabotropic glutamate receptor subtype 5 (mGluR5). VU0477573 exhibits neuroprotective and anxiolytic effects. VU0477573 can be used for the research of neurological disease, such as Parkinson disease .

Cat. No.	Product Name	Target	Research Area

HY-W101299

*N-Acetyl-D-allo-isoleucine*	Amino Acid Derivatives	Metabolic Disease
N-Acetyl-D-allo-isoleucine is an amino acid derivative. N-Acetyl-D-allo-isoleucine is promising for research of amino acid metabolism, such as abnormal isoleucine metabolism .

HY-P4910

Baceridin	Proteasome Apoptosis	Cancer
Baceridin is a proteasome inhibitor and a cyclic hexapeptide. Baceridin can be isolated from the culture medium of Epiphytic Bacillus. Baceridin can inhibit cell cycle progression and induce tumor cell apoptosis through a p53-independent pathway. Baceridin can be used in cancer research .

HY-P2120

Pseudobactin A	Bacterial	Others
Pseudobactin A is a non-fluorescent extracellular iron carrier produced by the plant growth-promoting bacterium Pseudomonas B10 .

HY-P11259

UPG-111	Urotensin Receptor	Cardiovascular Disease Metabolic Disease Inflammation/Immunology Cancer
UPG-111 is a peptide compound that acts as a negative allosteric modulator of the Urotensin II receptor (UTR). UPG-111 exhibits a dual inhibitory effect on the vasoconstriction induced by UTR agonists - it reduces both the maximum response intensity and the sensitivity of the agonist. UPG-111 does not induce calcium release or cause contraction of the endothelium-deprived rat aortic rings. UPG-111 can be used for the study of various diseases related to the angiotensinergic system .

HY-P4613

*Fmoc-D-allo-Thr-OH*	Drug Derivative Drug Intermediate	Others
Fmoc-D-allo-Thr-OH is a derivative of D-allothreonine (HY-W001959), which is commonly used as a building block in solid-phase peptide synthesis (SPPS) .

HY-P11022

TL-119 A-3302-B	Endogenous Metabolite HSV TRP Channel	Infection Cancer
TL-119 (A-3302-B) is a polypeptide. TL-119 can be isolated from the bacteria Micromonospora sp. MAG 9-7 and Saccharomonospora sp. CNQ-490. TL-119 inhibits TRPV-1. TL-119 exhibits antiviral activity against HSV-2. TL-119 possesses anticancer activity against gastric cancer and colorectal cancer .

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